Department of Pharmacy, Birla Institute of Technology & Science, Pilani, Rajasthan, India.
Indian J Pharmacol. 2013 May-Jun;45(3):248-51. doi: 10.4103/0253-7613.111923.
The present study was designed to investigate the anxiolytic activity of 6g, a novel serotonin type-3 receptor (5-HT3) receptor antagonist in experimental mouse models of anxiety.
The anxiolytic activity of "6g" (1 and 2 mg/kg, intraperitoneally [i.p.]) was evaluated in mice by using a battery of behavioral tests of anxiety such as elevated plus maze (EPM), light-dark (L&D) box, hole board (HB), and open field test (OFT) with diazepam (2 mg/kg, i.p.) as standard anxiolytic. None of the tested dose of "6g" affects the base line locomotion.
The new chemical entity "6g" (2 mg/kg, i.p.) and diazepam (2 mg/kg, i.p.) significantly (P < 0.05) increased the percentage of time spent and number of entries in open arm in the EPM test. In the L&D test compound "6g" (2 mg/kg, i.p.) and diazepam (2 mg/kg, i.p.) significantly (P < 0.05) increased the total time spent in light compartment as well as number of transitions from one compartment to other. Compound "6g" (1 and 2 mg/kg, i.p.) and diazepam (2 mg/kg, i.p.) also significantly (P < 0.05) increased number of head dips, whereas significantly (P < 0.05) decreased the head dipping latency in HB test as compared to vehicle control group. In addition, 6g (2 mg/kg, i.p.) and diazepam (2 mg/kg, i.p.) significantly (P < 0.05) increased the ambulation scores (square crossed) in OFT and there was no significant effect of 6g (1 and 2 mg/kg, i.p.) and diazepam (2 mg/kg, i.p.) on rearing scores.
In conclusion, these findings indicated that compound "6g" exhibited an anxiolytic-like effect in animal models of anxiety.
本研究旨在探讨新型 5-羟色胺 3 型受体（5-HT3）拮抗剂 6g 在焦虑实验小鼠模型中的抗焦虑活性。
通过一系列焦虑行为测试，如高架十字迷宫（EPM）、明暗（L&D）箱、洞板（HB）和旷场试验（OFT），评估“6g”（1 和 2 mg/kg，腹腔注射）在小鼠中的抗焦虑活性，并用安定（2 mg/kg，腹腔注射）作为标准抗焦虑药。测试剂量的“6g”均不影响基础运动。
新化学实体“6g”（2 mg/kg，腹腔注射）和安定（2 mg/kg，腹腔注射）显著（P<0.05）增加了 EPM 测试中开放臂的时间百分比和进入次数。在 L&D 测试中，化合物“6g”（2 mg/kg，腹腔注射）和安定（2 mg/kg，腹腔注射）显著（P<0.05）增加了亮室的总停留时间以及从一个室到另一个室的过渡次数。化合物“6g”（1 和 2 mg/kg，腹腔注射）和安定（2 mg/kg，腹腔注射）也显著（P<0.05）增加了头浸次数，而显著（P<0.05）降低了 HB 测试中的头浸潜伏期与对照组相比。此外，6g（2 mg/kg，腹腔注射）和安定（2 mg/kg，腹腔注射）显著（P<0.05）增加了 OFT 的走动分数（方格穿越），而 6g（1 和 2 mg/kg，腹腔注射）和安定（2 mg/kg，腹腔注射）对直立分数没有显著影响。
总之，这些发现表明化合物“6g”在焦虑动物模型中表现出抗焦虑样作用。
